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endocrine drugs

QuestionAnswer
Inhibitor of Na+-I- cotransporter PERCHLORATE
mechanism and main toxicity of perchlorate Block uptake of iodide (I-), Aplastic Anemia
Iodide mechanism Inhibit organification, Inhibit release of T3 and T4 (via inhibition of proteases), decrease size and vascularity of gland
Radioactive Iodine (131I) mechanism Rapid uptake of Iodine, Emission of radioactive β-particle Selective destruction of thyroid tissue
how toxic is radio active Iodine little to no toxicity
PROPYLTHIOURACIL (PTU) mechanism Block Organification, inhibit thyroid peroxidase
PROPYLTHIOURACIL is a Thioamide
Levothyroxine is t4 analogue
Ketoconazole is an antifungal
ketoconazole mechanism a non-selective inhibitor of steroid hormone biosynthesis. It inhibits various enzymes in the biosynthetic pathway of cortisol
Ketoconazole interacts with statins ex: simvastatin
Mifepristone GC receptor antagonist
Mitotane chemically non-selective adrenalectomic agent
OXYTOCIN actions Induces contraction of smooth muscle in reproductive tracts, initiating labor, stimulates lactation
DESMOPRESSIN ACETATE is a long synthetic vasopressin anologue, it has minimal vasoconstrictor effects. The Antidiuretic : Pressor ratio is 4000x higher than native ADH
CONIVAPTAN is ADH ANTAGONISTS: Used in patients with hyponatremia or acute HF. It has a high affinity for V1A and V2 rec
Chloropromide and Glyburide desctiption and MOA its a Sulfonylurea, which inhibits the atpase sensitive k channel
Chloropromide and Glyburide effect INCREASE insulin release from pancreas DECREASE Glucagon levels (mechanism unclear)
Chloropromide and Glyburide TOXICITY/SIDE EFFECTS Hypoglycemia (Most common side effect) Weight Gain Potentially Teratogenic
PRAMLINITIDE is Amylin Analog, a synthetic human amylin
MOA and effects Binds to the Amylin Receptor in specific regions of the brain. Activation of the amylin receptor cause reductions in glucagon release Promotes satiety, slows gastric emptying
PRAMLINITIDE Drug-Drug Interaction Contraindicated in patients with disorders of motility or on drugs that decrease gastric motility (i.e. OPIODE ANALGESICS)
REPAGLINIDE is Meglitinides
REPAGLINIDE MOA STIMULATE insulin release from pancreas Similar mechanism to sulfonylureas
NATEGLINIDE is d-phenylalanine derivative
NATEGLINIDE MOA STIMULATE insulin release from pancreas Similar mechanism to sulfonylureas
NATEGLINIDE and REPAGLINIDE adverse effects Hypoglycemia, diarrhea, nausea and weight gain
Metformin is a Biguanide that activates ampk
METFORMIN effects Liver: Decreases gluconeogenesis Skeletal muscle: Increase glucose utilization (lowers glucose levels) DOES NOT DEPEND ON FUNCTIONING PANCREATIC BETA CELLS
Metformin adverse effects and metabolism IMPAIRS HEPATIC LACTIC ACID METABOLISM Lactic acidosis Muscle pain Metabolism: Not metabolized Excreted unchanged in the urine
PIOGLITAZONE Insulin Sensitizer: Thiazolidinediones (TZD’s)
PIOGLITAZONE MOA acts on PPAR GAMMA INCREASE INSULIN SENSITIVITY DECREASE INSULIN RESISTANCE INCREASE GLUCOSE UTILIZATION
PIOGLITAZONE adverse effects ASSOCIATED WITH BLADDER CANCER FLUID RETENTION
ACARBOSE ALPHA-GLUCISIDASE INHIBITOR
ACARBOSE MOA Inhibit α-glucosidase in GI tract Decrease absorption of Glucose
Acarbose GI disturbance Excess carbohydrates in GI tract lead to increased bacterial digestion of polysaccharides. Contraindicated in people with Inflammatory Bowel Disease
EXENATIDE GLUCAGON-LIKE PEPTIDE-1 (GLP-1) RECEPTOR AGONISTS
EXENATIDE effects promotes: STIMULATES INSULIN PRODUCTION REDUCES APPETITE INDUCES β-CELL GROWTH
EXENATIDE adverse effects GI disturbance
SITAGLIPTIN DIPEPTIDYL PEPTIDASE-4 (DPP-4) INHIBITOR
sitagliptin effects INCREASE CIRCULATING GLP-1 INCREASE INSULIN LEVCELS DECREASE GLUCAGON LEVELS Adverse effects: GI disturbance
CANAGLIFLOZIN Sodium-Glucose transporter inhibitor (SGLT-2 inhibitor)
Canagliflozin MOA Inhibits the reabsorbtion of glucose Results in loss of glucose (glycosuria) and water (osmotic diuresis)
Canagliflozin Adverse effects Increased urination Increased urinary tract infections Possible hypotension
SIMVASTATIN is a prodrug, absorbed in the small intestine, and activated in the liver
DRUGS THAT INTERFERE WITH STATIN OXIDATION Macrolide antibiotics: e.g. Erythromycin Azole antifungals: e.g. Itraconazole Cyclosporine (immunosuppressant) Nefazodone (a phenylpiperazine antidepressant) HIV protease inhibitors Amiodarone (Antiarrhythmic agent)
Adverse effects of statins (simvastatin) MYOPATHY The major adverse effect associated with statin use Statin-induced rhabdomyolysis Risk increased in proportion to dose and plasma concentrations Associated with factors inhibiting statin catabolism
CHOLESTYRAMINE Bile-Acid Sequestrant
CHOLESTYRAMINE MOA Positively charged compounds IONIC BOND with negatively charged bile acids Block reabsorbtion and enhance excretion of cholesterol ENHANCES bile acid synthesis  reduces hepatic cholesterol → INC LDL-R synthesis
CHOLESTYRAMINE adverse Relatively safe Interfere with absorption of other drugs FUROSEMIDE, THIAZIDE DIURETICS,PROPRANOLOL, DIGOXIN, WARFARIN
niacin MOA Inhibits hormone-sensitive lipase DECREASES hepatic TG synthesis Decreases VLDL production and release Decreases HDL breakdown
Niacin ADVERSE EFFECTS Cutaneous vasodilation (flush) A prostaglandin dependent phenomena Treated with NSAIDs, salicylate-containing creams (i.e. Aspercreme™) and aspirin Dyspepsia May increase insulin resistance
CLOFIBRATE MOA Act as PPARα ligands
Clofibrate effects Increased FFA OXIDATION Increased expression and release of ApoA1 INC expression of LPL ↓ HEPATIC VLDL SECRETION, ↓ TGs, modest ↓ LDL, ↑ HDL
Clofibrate adverse effects Displace oral anticoagulants from protein binding sites. Myopathy when combined w/ statins (gemfibrozil only) Gemfibrozil blocks OATP1B1 transporter Associated w/ gallstone formation
EZETIMIBE MOA Inhibits luminal cholesterol uptake in the SMALL INTESTINE Decreases cholesterol uptake into chylomicrons Reduces cholesterol in liver Increases LDL-Receptor expression Inc plasma LDL clearance
Ezetimibe interactions BILE ACID SEQUESTRANTS INHIBIT ABSORBTION (ex: cholestyramine) CONTRAINDICATED No other interaction reported
ALIROCUMAB is a pcsk9 inhibitor. ( PCSK9 inhibitors have been shown to reduce LDL levels by up to 60 percent from baseline levels, (including in statin-intolerant)
ALIROCUMAB MOA Binds and inactivates PCSK9 Inhibits degradation of LDL-R Increases LDL-R number
ALIROCUMAB adverse effect Itching and swelling at site of injection Flu-like symptoms Hypersensitivity-type reactions
Somatotropin is Identical to human GH
Mecasermin recombinant human IGF-I (rh IGF-I) - Used for treatment of GH-resistant IGF-I deficiency
Octreotide Somatostatin analog
Pegvisomant GH receptor anatgonist, Binds only to one GH receptor, will stop dimerization
Created by: ksoul6